This is a national phase filing of the Application No. PCT/DE96/02487, which was filed with the Patent Corporation Treaty on Dec. 20, 1996, and is entitled to priority of the German Patent Application 195 48 114.3, filed Dec. 21, 1995.
The present invention relates to conjugates, comprising an active substance, a polypeptide and a polyether, a process for the preparation of such conjugates as well as their use.
There is a great demand of concentrating active substances at their site of action. This applies particularly to active substances for treating tumors and inflamed tissues, respectively. It is very often tried to obtain the active substance concentration by administration of high amounts of active substance. However, this leads to considerable side-effect in patients, particularly in their livers and kidneys.
Therefore, it is the object of the present invention to provide a possibility of concentrating active substances at their site of action.
The present invention relates to conjugates, comprising an active substance, a polypeptide and a polyether, a process for the preparation of such conjugates as well as their use.
4. BRIEF DESCRIPTION OF THE DRAWINGS
FIG. 1 shows a conjugate according to the invention, comprising polylysine (PL), 4 polyethylene glycols (PEG), 8 aminofluoresceins (AF1) and 2 diethylenetriaminepentaacetates (DTPA) labeled with 111In, AF1 being linked via cyanuric chloride to free amino groups of PL, and DTPA being linked to PL via an acid amide bridge (SEQ ID NO:1).
FIG. 2 shows the distribution of the conjugate of FIG. 1 according to the invention, measured by means of scintiscanning, in tumor tissue.